Abstract: An organic layer prepared from the seed of Aceriphyllum rossii was studied to identify the active compounds for protein tyrosine phosphatase 1B (PTP1B) inhibition. Bioassay guided fractionation resulted in the isolation of PTP1B inhibitory activity of triterpenes (1-4). These four compounds were identified as aceriphyllic acid C (1), aceriphyllic acid D (2), aceriphyllic acid E (3) and aceriphyllic acid F (4). The isolated 1-4 compounds inhibited PTP1B with IC₅₀ values ranged from (2.1±1.5) μmol/L to (11.2±2.5) μmol/L. Kinetic analysis of PTP1B inhibition by aceriphyllic acid C (1) and aceriphyllic acid D (2) suggested that oleanane-type triterpenes inhibited PTP1B activity in a mixed-type manner.

Key words: Aceriphyllum rossii, Protein tyrosine phosphatase 1B, Triterpenes, Bioassay guided